title: Aminopyrazinoic acid esters as potential antimycobacterial drugs.
abstract: A series of esters of the 3-aminopyrazine-2-carboxylic acid as potential antimycobacterial drugs was synthesized. A CEM Discover microwave reactor with an autosampler Explorer 24 which served to accelerate the reaction was used for synthesis. The prepared products were characterized by IR, 1H NMR, 13C NMR spectra, elementary analysis and melting points. Log P and ClogP values were calculated. Final products were evaluated in vitro for their antimycobacterial activity. The most active compound was hexyl 3-aminopyrazine-2-carboxylate (7), whose antimycobacterial activity (MIC) against M. tuberculosis H37Rv was 6.25 μg/mL.
authors.affiliation: Charles University in Prague, Faculty of Pharmacy, Department of Heyrowského, Czech Republic. martin.dolezal@faf.cuni.cz
authors.forename: Martin
authors.initials: M
authors.lastname: Doležal
authors.forename: Jana
authors.initials: J
authors.lastname: Vobicková
authors.forename: Barbora
authors.initials: B
authors.lastname: Servusová
authors.forename: Pavla
authors.initials: P
authors.lastname: Paterová
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004952:Esters; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000995:Antitubercular Agents; D004952:Esters; D011719:Pyrazines; C016227:3-aminopyrazine-2-carboxylic acid